Synthesis and optimization of a reactive oxygen species responsive cellular delivery system

Abstract

Reactive oxygen species play numerous roles in a number of pathological processes. Monitoring H₂O₂ is a powerful tool for imaging and therapy of diseases wherein oxidative stress is involved. In particular, we report a specific application of functional microspheres as sensors of H₂O₂. Reactive oxygen species responsive delivery systems were developed to detect in vitro peroxides thanks to the presence of a boronic ester which is readily cleaved with H₂O₂. This ROS-sensitive cleavable linker underwent a 1,6-elimination to disrupt fluorescence resonance energy transfer by coupled near-infrared fluorophores such as Cy5.5/Cy7. This technology would allow real-time monitoring of therapeutic regimes (and their success), as well as optical detection of inflammation.